Abarelix is a synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It directly and competitively binds and blocks the gonadotropin releasing hormone receptors in the anterior pituitary, which inhibits the secretion and release of the luteinizing hormone (LH) and follicle stimulating hormone (FSH). For men, the inhibition of LH secretion prevents the release of testosterone. Therefore, it can relieve symptoms associated with prostate hypertrophy or prostate cancer.
CAT No: 10-101-60
CAS No:183552-38-7
Synonyms/Alias:Abarelix;183552-38-7;Plenaxis;PPI-149;Plenaxis depot;PPI 149;R 3827;R-3827;UNII-W486SJ5824;CHEBI:337298;R3827;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-;CHEMBL1252;PPI149;DTXSID20171443;W486SJ5824;N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N(sup 6)-isopropyl-L-lysyl-L-prolyl-D-alaninamide;R382;R-382;N-acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(pyridin-3-yl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparginyl-L-leucyl-N(6)-isopropyl-L-lysyl-L-prolyl-D-alaninamide;Abarelix-Depot-M;Abarelix Trifluoroacetate Salt (~90%);Plenaxis (TN);Abarelix (USAN/INN);Abarelix [USAN:INN];abarelixum;N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparginyl-L-leucyl-N6-isopropyl-L-lysyl-L-prolyl-D-alaninamide;SCHEMBL9533;GTPL1188;DTXCID4093934;SCHEMBL19712245;L02XB01;AIWRTTMUVOZGPW-HSPKUQOVSA-N;Abarelix acetate - Bio-X trade mark;BDBM50102442;AKOS040732360;R3827;PPI 149;AT36700;CS-5873;DB00106;FA55835;BA300028;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl- 10;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-10;HY-13534;MS-32159;D02738;EN300-20605823;Q305555;Ac-D-Nal-[D-(pCl)Phe]-D-Pal-Ser-[Nalpha-Me-Tyr]-D-Asn-Leu-ILys-Pro-DAla-NH2;N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N(6)-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide;
Chemical Name:(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]-methylamino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-6-(propan-2-ylamino)hexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]butanediamide
Abarelix is a synthetic decapeptide that functions as a gonadotropin-releasing hormone (GnRH) antagonist, designed to modulate the hypothalamic-pituitary-gonadal axis by competitively inhibiting endogenous GnRH receptor activation. As a peptide-based research compound, it is characterized by its ability to rapidly suppress luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion, resulting in effective downregulation of gonadal steroidogenesis. The unique structure and receptor-binding profile of abarelix make it a valuable tool in studies focused on hormonal regulation, endocrine signaling, and the molecular pharmacology of peptide antagonists. Its utility extends across a range of biochemical investigations where precise manipulation of GnRH-mediated pathways is required.
Endocrine signaling research: Abarelix is widely utilized as a reference GnRH antagonist in studies dissecting the molecular mechanisms of pituitary hormone release. By providing a means to selectively block GnRH receptor activation, it enables researchers to investigate the downstream effects on LH and FSH synthesis and secretion. This targeted approach is essential for elucidating the feedback loops and regulatory checkpoints within the hypothalamic-pituitary-gonadal axis, supporting a deeper understanding of endocrine physiology and pathophysiology.
Reproductive biology studies: The compound serves as a critical reagent in experiments that require suppression of gonadal steroid production, such as investigations into spermatogenesis, ovarian function, or the hormonal regulation of reproductive cycles. By inducing rapid and reversible inhibition of gonadotropin release, abarelix allows for controlled experimental conditions that facilitate the study of reproductive tissue responses, gametogenesis, and the interplay between steroid hormones and their target organs.
Peptide antagonist pharmacology: As a model GnRH antagonist, abarelix is frequently employed in structure-activity relationship (SAR) analyses and receptor binding assays. Its well-characterized interaction with the GnRH receptor provides a benchmark for assessing the potency, selectivity, and efficacy of novel peptide analogs or small-molecule antagonists. Such studies are instrumental in advancing the rational design of next-generation GnRH modulators and in mapping key structural determinants required for receptor blockade.
Signal transduction pathway analysis: Researchers leverage abarelix to delineate the intracellular signaling cascades triggered by GnRH receptor antagonism. By selectively interrupting receptor-mediated activation, it becomes possible to monitor changes in second messenger systems, kinase activation patterns, and gene expression profiles. These investigations contribute to a comprehensive understanding of how peptide antagonists reprogram cellular responses and modulate endocrine cell function at the molecular level.
Animal model development: In preclinical research, abarelix is incorporated into animal studies to transiently suppress gonadotropin and steroid hormone levels, creating models of hormonal ablation. Such models are invaluable for probing the physiological consequences of endocrine disruption, validating biomarkers of hormone deprivation, and exploring the effects of hormonal manipulation on target tissues. The precise and predictable action of abarelix supports reproducible experimental outcomes in complex in vivo systems.
3. SERS spectrum of the peptide thymosin‐β4 obtained with Ag nanorod substrate
4. Myotropic activity of allatostatins in tenebrionid beetles
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